Lead optimization efforts resulted in the discovery of two potent, selective, and orally
bioavailable PI3Kδ inhibitors, 1 (AM-8508) and 2 (AM-9635), with good pharmacokinetic …

Optimization of the potency and pharmacokinetic profile of 2, 3, 4-trisubstituted quinoline, 4,
led to the discovery of two potent, selective, and orally bioavailable PI3Kδ inhibitors, 6a (AM …

Optimization of the potency and pharmacokinetic profile of 2, 3, 4-trisubstituted quinoline, 4,
led to the discovery of two potent, selective, and orally bioavailable PI3Kδ inhibitors, 6a (AM …

Structure-based rational design led to the synthesis of a novel series of potent PI3K
inhibitors. The optimized pyrrolopyridine analogue 63 was a potent and selective PI3Kβ/δ …

PI3Kδ catalytic activity is required for immune cell activation, and has been implicated in
inflammatory diseases as well as hematological malignancies in which the AKT pathway is …

Optimization of a previously reported lead series of PI3Kδ inhibitors with a novel binding
mode led to the identification of a clinical candidate compound 31 (GSK251). Removal of an …

Phosphoinositide 3-kinase δ (PI3Kδ) plays a critical role in B lymphocyte (B-cell)
development and activation and has been a validated target for the treatment of B-cell …

Abstract Aberrant Class I PI3K signaling is a key factor contributing to many immunological
disorders and cancers. We have identified 4-amino pyrrolotriazine as a novel chemotype …

Inhibition of PI3Kδ is considered to be an attractive mechanism for the treatment of
inflammatory diseases and leukocyte malignancies. Using a structure-based design …

In the recent years, PI3Kδ has emerged as a promising target for the treatment of B-and T-
cell mediated inflammatory diseases. We present a cellular assay activity analysis for our …